The pharmacology of isamoxole [2-methyl-n-butyl-n(4-methyloxazol-2-yl) propanamide] LRCL 3950, a new anti-allergic compound.
1. Isamoxole [2-methyl-N-butyl-N(4-methyloxazol-2-yl) propanamide] is an effective orally active anti-allergic compound in animals. 2. Isamoxole inhibits the immunological release of mediators, notably slow-reacting substance of anaphylaxis (SRS-A) from sensitized human and guinea-pig chopped lung in vitro. 3. In vivo, allergic responses were inhibited in guinea-pigs and rats by doses as low as 25 mg/kg given orally 180 and 30 min before challenge. The effect of Isamoxole was still present 4 h after a single dose of 100 mg/kg orally in the guinea-pig and 3 h in the rat. 4. Isamoxole is a moderately potent, selective inhibitor of SRS-A activity on the guinea-pig ileum in vitro, at concentrations that do not antagonize histamine, 5-hydroxytryptamine, or bradykinin. 5. Isamoxole causes human bronchial muscle to relax and antagonizes the bronchoconstriction induced by SRS-A.
D000818:Animals; D001986:Bronchial Spasm / Q000517:prevention & control; D001993:Bronchodilator Agents; D016861:Cyclooxygenase Inhibitors; D006168:Guinea Pigs; D006801:Humans; D006967:Hypersensitivity / Q000188:drug therapy*; D066298:In Vitro Techniques; D008168:Lung / Q000378:metabolism; D008297:Male; D010080:Oxazoles / Q000494:pharmacology*; D010323:Passive Cutaneous Anaphylaxis / Q000187:drug effects; D010726:Phosphodiesterase Inhibitors; D051381:Rats; D013189:SRS-A / Q000378:metabolism
D001993:Bronchodilator Agents; D016861:Cyclooxygenase Inhibitors; D010080:Oxazoles; D010726:Phosphodiesterase Inhibitors; D013189:SRS-A; C017436:isamoxole